1-(吡啶-4-基)环丁胺 | 1211593-50-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 1-(吡啶-4-基)环丁胺
• 英文名称: 1-(pyridin-4-yl)cyclobutan-1-amine
• 英文别名: 1-pyridin-4-ylcyclobutan-1-amine
• CAS: 1211593-50-8；1212058-00-8
• 化学式: C₉H₁₂N₂
• 分子量: 148.208
• InChiKey: IDWHILRTFFJHIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(吡啶-4-基)环丁胺 、 5-[(3R)-5’,6’-dihydrospiro[pyrrolidine-3,4’-pyrrolo[1,2-b]pyrazol]-2’-yl]-3-(trifluoromethyl)pyridin-2-amine hydrogen chloride 、 N,N'-羰基二咪唑 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 10.0h， 生成 (3R)-2’-[6-amino-5-(trifluoromethyl)pyridin-3-yl]-N-[1-(pyridin-4-yl)cyclobutyl]-5’,6’-dihydrospiro[pyrrolidine-3,4’-pyrrolo[1,2-b]pyrazole]-1-carboxamide
  参考文献：
  名称：

  [EN] MAP4K1 INHIBITORS
  [FR] INHIBITEURS DE MAP4K1

  摘要：

  本发明涉及公式（I）（I）的Map4K1抑制剂，其中A，E，G，Q，R1，R2和R4的含义与说明中定义的相同，涉及包含根据本发明的化合物的制药组合物和组合物，以及创新化合物的预防和治疗用途，分别用于制造用于治疗或预防疾病的制药组合物，特别是用于肿瘤性疾病，或与异常MAP4K1信号相关的其他紊乱免疫反应或其他疾病，作为唯一药物或与其他活性成分联合使用。本发明还涉及用于制造用于治疗或预防良性增生，动脉粥样硬化疾病，败血症，自身免疫性疾病，血管疾病，病毒感染，神经退行性疾病，炎症性疾病，动脉粥样硬化疾病和男性生育控制的制药组合物的使用，分别使用上述化合物制造制药组合物。

  公开号：

  WO2022167627A1

文献信息

• CANNABINOID RECEPTOR MODULATORS
  申请人：Jones Robert M.

  公开号：US20120214766A1

  公开（公告）日：2012-08-23

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

  本发明涉及公式Ia的某些化合物及其制药组合物，其调节大麻素CB2受体的活性。本发明还涉及公式Ia的某些化合物及其制药组合物，其调节CB1受体和CB2受体的活性。本发明的化合物和制药组合物适用于治疗以下疾病的方法：疼痛，例如骨骼和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛，炎性疼痛，神经痛，由治疗副作用引起的疼痛和与骨关节炎相关的疼痛；过敏症；炎性过敏症；神经病性过敏症；急性疼痛感受；骨质疏松症；多发性硬化症相关痉挛；自身免疫疾病；过敏反应；中枢神经系统炎症；动脉粥样硬化；不良的免疫细胞活动和炎症；年龄相关的黄斑变性；咳嗽；白血病；淋巴瘤；中枢神经系统肿瘤；前列腺癌；阿尔茨海默病；中风引起的损伤；痴呆症；肌萎缩性侧索硬化症和帕金森病。
• Cannabinoid receptor modulators
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US11214548B2

  公开（公告）日：2022-01-04

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

  本发明涉及某些调节大麻素 CB2 受体活性的式 Ia 化合物及其药物组合物。本发明还涉及某些能调节 CB1 受体和 CB2 受体活性的式 Ia 化合物及其药物组合物。本发明的化合物及其药物组合物用于治疗以下疾病的方法：疼痛，例如骨痛和关节痛、肌肉痛、牙痛、偏头痛和其他头痛、炎症性疼痛、神经性疼痛、作为治疗药物的不良反应出现的疼痛以及与骨关节炎相关的疼痛；痛觉减退；异动症；炎症性痛觉减退；神经性痛觉减退；急性痛觉；骨质疏松症；多发性硬化症相关的痉挛、自身免疫性疾病、过敏反应、中枢神经系统炎症、动脉粥样硬化、不想要的免疫细胞活性和炎症、老年性黄斑变性、咳嗽、白血病、淋巴瘤、中枢神经系统肿瘤、前列腺癌、阿尔茨海默病、中风引起的损伤、痴呆、肌萎缩性脊髓侧索硬化症和帕金森病。
• COMPOUNDS AND METHODS FOR TREATMENT OF VISCERAL PAIN
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP3621619A1

  公开（公告）日：2020-03-18
• Compounds and Methods for Treatment of Visceral Pain
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US20200078358A1

  公开（公告）日：2020-03-12

  The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof and their use in methods for the alleviation and/or treatment of visceral pain, for example abdominal pain; pelvic pain; male pelvic pain; pain from an internal organ; bladder pain; painful bladder syndrome; post-surgical abdominal pain (e.g., GI resection, hysterectomy, oophorectomy, C-section, and the like); or pain arising from or related to: pancreatitis (e.g., chronic pancreatitis), prostatitis (e.g., chronic prostatitis), inflammatory bowel disease (e.g., Crohn's disease), endometriosis, interstitial cystitis, prostatitis (e.g., chronic prostatitis), epididymitis (e.g., chronic epididymitis), or post-surgical abdominal lesions. In some embodiments, the visceral pain is consequent to inflammatory bowel disease, for example Crohn's disease.
• US8778950B2
  申请人：——

  公开号：US8778950B2

  公开（公告）日：2014-07-15